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SMA-pirarubicin
- Development stage
- Unknown
- Lead developer
- University of Melbourne
- Modality
- Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
SMA-pirarubicin is a polymer-conjugated micellar formulation of the anthracycline cytotoxic antibiotic pirarubicin (4'-O-tetrahydropyranyladriamycin). It utilizes a styrene-maleic acid (SMA) copolymer to encapsulate the drug, leveraging the Enhanced Permeability and Retention (EPR) effect for tumor-targeted delivery. This formulation is designed to increase the plasma half-life of pirarubicin and improve its accumulation in tumor tissues, particularly liver metastases, while reducing systemic toxicities such as cardiotoxicity. Mechanistically, it acts as a topoisomerase II inhibitor and DNA intercalator, leading to DNA strand breaks and apoptosis in cancer cells. Preclinical research has shown that treatment with SMA-pirarubicin can induce significant tumor damage and acute hypoxia, which may trigger a transient epithelial-to-mesenchymal transition (EMT) in surviving tumor cells as a protective stress response.
- Other names
- SMA-pirarubicin micellesStyrene-maleic acid copolymer-pirarubicinSMA-THP micelles
02
Targets
TOP2A (DNA topoisomerase II)DNA
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